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New thienopyridine compound

A technology for compounds and diseases, used in organic chemistry, drug combinations, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2013-03-27
GUANGDONG ZHONGKE DRUG R&D
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, this type of drug is widely used in the world, but it is more appropriate as a preventive drug than a therapeutic drug, because the effect of using this type of drug in the acute stage of stroke is not ideal

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: the preparation of each compound:

[0020] Because the compounds described herein have strong coherence, in order to describe the preparation method of each compound in detail, accurately and conveniently, it is expressed with 1 embodiment, and the serial number of the compound is indicated below each compound of the following synthetic route, for more Concise descriptions are replaced by serial numbers in the following preparation methods:

[0021]

[0022] Different compounds 11a, 11b, 11c, 11b and 11e are obtained when R is a different group in the above scheme.

[0023] (1), the synthesis of compound 2:

[0024] Dissolve 154 grams of compound 1 and 220 grams of triethylamine in 500 mL of THF, add 142 grams of thionyl chloride dropwise under ice-cooling, complete the dropwise addition within 30 minutes, continue the reaction for 30 minutes, and then move the reaction solution to room temperature React for one hour, then reflux for another hour, coo...

Embodiment 2

[0043] In the same way, R 1 -Cl, R 2 Each compound when it is a different organic acid or inorganic acid. Example 2: Effects on Cerebral Infarction Volume in Rats with Focal Cerebral Ischemia

[0044] (1) Experimental materials and methods

[0045] Wistar rats, body weight 250-280g. They were reared separately before and after the operation, the room temperature was kept at 23-25°C, and they had their own food and water. The tMCAO model was prepared according to the method of Longa et al. The rats were anesthetized with 10% chloral hydrate (350mg / kg, i.p.), the body temperature was maintained at 37±0.5°C, and they were fixed on the operating table in a supine position. The skin was cut along the midline of the neck, and the right common carotid artery (CCA), external carotid artery (ECA), and internal carotid artery (ICA) were carefully separated. Cut the ECA ligation and straighten it to be in line with the ICA. Cut a small opening on the ECA, and insert a 4.0cm-long, ...

Embodiment 13

[0056] Example 13: Effects of compound 10, compound 11a and 11b on sleep in rats:

[0057] (1) Sleep improvement test

[0058] Animal source: Kunming white mice, 18-22 grams, male, clean animals provided by Guangdong Experimental Animal Center. The temperature of the experimental animal breeding room is 22±2°C, the relative humidity is 50-70%, and the animal feed is provided by Guangdong Experimental Animal Center.

[0059] In this experiment, three groups of compounds 10, 11a, and 11b were set up at 25 mg / kg respectively, and a distilled water control group was also set up.

[0060] Sample treatment: Take 25mg of each sample and add distilled water to 20ml to make a uniform suspension for testing.

[0061] Way of giving samples: gavage

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Abstract

The invention discloses a new thienopyridine compound (shown in a formula I) and a salt thereof. Experiments prove that the new thienopyridine compound can be used for treating and preventing ischemic disease and improving sleep. When R2 represents H, the new thienopyridine compound can react with organic acids (such as phosphoric acid, hydrogen nitrate and sulfuric acid) and organic acids (such as methanoic acid, acetic acid, propanoic acid, oxalic acid, malonic acid, aminoacetic acid, valine, maleic acid, fumaric acid and succinic acid) to generate ester, and further react with acid or basic group to generate a salt. The salt also has the functions of treating and preventing ischemic disease and improving sleep.

Description

technical field [0001] The invention belongs to the medical field of compounds, relates to a new compound of pyridothiophene and its salt, and discloses its preparation method and application. Background technique [0002] Cerebral infarction in a broad sense refers to the sudden decrease in blood perfusion or complete interruption of blood flow in local blood supply arteries of brain tissue, stopping blood supply, oxygen supply, sugar supply, etc., causing the local brain tissue to disintegrate and destroy. The main causes of ischemic stroke are: ①thromboembolism caused by atherosclerosis; ②cerebral embolism caused by emboli from the heart; ③vasculitis, vascular injury and trauma caused by various reasons. Ischemic stroke usually occurs during sleep at night, often when you wake up in the next morning, you will find limb weakness or hemiplegia, often without disturbance of consciousness, blood pressure can be normal or high, and there may be a history of arteriosclerosis. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D495/04A61K31/4365A61P9/10A61P25/20
Inventor 苏春华
Owner GUANGDONG ZHONGKE DRUG R&D
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